Udenafil is the fourth in a class of drugs targeting the inhibition of the enzyme phosphodiesterase 5 (PDE5) for the treatment of erectile dysfunction. Inhibition of PDE5 results in the increase in endogenous cyclic guanosine monophosphate (cGMP) concentrations in the penile corpus cavernosum. cGMP induces smooth muscle cell relaxation and subsequent increased blood flow leading to a sustainable erection. Udenafil is a potent antagonist of human PDE5 with an IC50 of 8.25nM and a comparable selectivity profile as sildenafil for the other PDEs. Unlike tadalafil, it does not inhibit PDE11, which has been implicated in myalgia and testicular toxicity. Furthermore, udenafil produced up to a 91% vaginal penetration success rate and up to a 67% intercourse completion rate compared to a 29% completion rate by placebo. Overall patient satisfaction, measured by a standard global assessment question, was 86% compared to only 26% in the placebo group. The most frequently recorded adverse events were mild-to-moderate facial flushing and headache.
Udenafil is an inhibitor of phosphodiesterase 5 (PDE5). In vivo, udenafil (1 and 5 mg/kg) increases lung cGMP levels, attenuates the development of compensatory right ventricular hypertrophy, and reduces pulmonary arterial wall thickening in a rat model of monocrotaline-induced pulmonary hypertension. It increases creatine clearance and decreases blood urea nitrogen (BUN) and serum malondialdehyde (MDA) levels in a rat model of renal ischemia-reperfusion injury. Udenafil (0.3 and 10 mg/kg) induces penile erections in conscious rabbits and in rabbits with acute spinal cord injury.
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Product Name: | Udenafil |
Synonyms: | 5-[2-propyloxy-5-(2-(1-Methylpyrrolidin-2-yl)ethylaMinosulphonyl)phenyl]-1-Methyl-3-propyl-6,7-dihydro-1H-pyrazolo(4,3-d)pyriMidin-7-one;5-[2-propyloxy-5-[2-(1-Methyl-2-pyrrolidinyl)ethylaMinosulfonyl]phenyl]-1-Methyl-3-propyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyriMidine-7-one;Zydena;Udenafil(DA 8159,Zydena);BenzenesulfonaMide,3-(6,7-dihydro-1-Methyl-7-oxo-3-propyl-1H-pyrazolo[4,3-d]pyriMidin-5-yl)-N-[2-(1-Methyl-2-pyrrolidinyl)ethyl]-4-propoxy-;Udenafil, DA 8159;CS-1353;Udenafil, >=98% |
CAS: | 268203-93-6 |
MF: | C25H36N6O4S |
MW: | 516.66 |
EINECS: | 251-228-4 |
Product Categories: | Intermediates & Fine Chemicals;Pharmaceuticals |
Mol File: | 268203-93-6.mol |
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Udenafil Chemical Properties |
熔点 | 152-159°C |
沸点 | 697.0±65.0 °C(Predicted) |
密度 | 1.35 |
储存温度 | under inert gas (nitrogen or Argon) at 2-8°C |
溶解度 | Chloroform (Slightly), Methanol (Sparingly) |
形式 | Solid |
pka | 11.07±0.50(Predicted) |
颜色 | White to Pale Beige |
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